[EN] N-PYRAZOLYL CARBOXAMIDES AS CRAC CHANNEL INHIBITORS<br/>[FR] CARBOXAMIDES N-PYRAZOLYL EN TANT QU'INHIBITEURS DU CANAL CRAC
申请人:GLAXO GROUP LTD
公开号:WO2010122089A1
公开(公告)日:2010-10-28
The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
Use of the cascade α-oxo-amidoalkylation/transposition/ p-cationic cyclization of N-acyliminium ions in the synthesis of novel fused heterocyclic N,O-acetals
作者:Adam Daïch、Anthony Pesquet、Luc Van Hijfte
DOI:10.3998/ark.5550190.0011.805
日期:——
Tricyclic N,O-acetal scaffolds have been prepared easily in few steps starting from cheap reagents in moderate to good yields (40-68%) in which the α-hydroxy lactam intermediates constitute the key substrates. These cyclized products are the result of the exclusive intramolecular attack of the oxygen atom onto the endocyclic N-acyliminiumion intermediates leading to the new cyclic aza-oxonium salts
Acidic Rearrangement of (Benzyloxy)chalcones: A Short Synthesis of Chamanetin
作者:Gustavo Seoane、Gabriel Sagrera
DOI:10.1055/s-0029-1217064
日期:——
Treatment of (benzyloxy)chalcones with trifluoroacetic acid in refluxing chloroform gave several new benzyl(hydroxy)flavanones in high yields and good regioselectivities. By using this procedure, we prepared the natural compound chamanetin in good yield from readily available reagents. benzylation - rearrangements - protecting groups - chamanetin - chalcones
The invention provides compounds of formula (I) and salts thereof: R
1
-L-R
2
—B wherein R
1
, L, R
2
, and B have any of the values defined herein, as well as compositions comprising such compounds, and therapeutic methods comprising the administration of such compounds or salts. The compounds block siderophore production in bacteria and are useful as antibacterial agents.
An aryne triggered ring-opening fluorination of cyclic thioethers with potassium fluoride
作者:Rong Fan、Binbin Liu、Tianyu Zheng、Kun Xu、Chen Tan、Tianlong Zeng、Shuaisong Su、Jiajing Tan
DOI:10.1039/c8cc03766c
日期:——
report an aryne triggered ring-opening fluorination protocol of a great variety of saturated sulfur heterocycles. A key factor for the success is the identification of a suitable mediator. Compared to previous methods, this transition-metal free protocol employs low-cost potassium fluoride as the fluorine source. The operational simplicity and mild reaction conditions allow for the rapid synthesis of a